Search results for " High pressure liquid"

Bis(hydroxyphenyl)methane-bisphenol F-metabolism by the HepG2 human hepatoma cell line and cryopreserved human hepatocytes

2011

author cannot archive publisher's version/PDF; International audience; Bisphenol F (BPF) is present in the environment and as a contaminant of food. Humans may, therefore, be exposed to BPF, and an assessment of this risk is required. BPF has been shown to have genotoxic and endocrine-disruptor properties in a human hepatoma cell line (HepG2), which is a model system for studies of xenobiotic toxicity. In this study, we investigated the ability of HepG2 cells to biotransform BPF, because metabolism may affect the observed effects of BPF, and we compared this metabolic capacity with that of human hepatocytes. Cells were incubated for 24 hours with [(3)H]-BPF. The culture medium was then conc…

Adrenic acid Δ4 desaturation and fatty acid composition in the liver of marine-oil fed streptozotocin diabetic rats

1998

The aim of the present study was to assess the effect of streptozotocin diabetes and insulin treatment on adrenic acid delta4 desaturation and fatty acid composition of liver microsomes in Wistar rats fed a fat free semi-synthetic basal diet supplemented with 10% EPA-rich marine oil. Results showed that, in liver microsomes of hyperglycemic rats, the 22:6n-3/22:5n-3 ratio in total lipids was elevated and desaturation of adrenic acid to n-6 docosapentaenoic acid was enhanced. Insulin treatment with 2.0 I.U./100 g body weight-1 twice a day for 3 days resulted in hypoglycemia and suppressed both the increased delta4 n-6 desaturation and 22:6n-3/22:5n-3 ratio. It is concluded that the delta4 de…

Bone status in adolescents with type 1 diabetes

2010

Aims The aim of the study was to investigate the potential negative impact of type 1 diabetes on bone status of adolescents. Bone status in adolescents with type 1 diabetes was assessed by means of quantitative ultrasound (QUS) and the influence of metabolic control and other diseaserelated and growth variables was analysed. Methods Group I consisted of 99 pubertal (Tanner ≥2) adolescents (49 female), aged 14.3±2.5 years, diabetes duration 4.6±2.3 years. Controls (group II) were 297 children, matched by sex and age, from a healthy population. The influence of glycated haemoglobin (current: HbA1cD; last year’s mean: HbA1cY; whole duration mean: HbA1cT), diabetes duration, percentage of life …

Cyclooxygenase-1/2 (COX-1/COX-2) and 5-lipoxygenase (5-LOX) inhibitors of the 6,7-diaryl-2,3-1H-dihydropyrrolizine type

2003

A series of 6,7-diaryl-2,3-1H-dihydropyrrolizines was prepared as COX-1/COX-2 and 5-LOX inhibitors. The inhibition of COX-1 was evaluated using intact bovine platelets as the enzyme source, whereas LPS-stimulated human monocytes served as the enzyme source for inducible COX-2. The determination of arachidonic metabolites was performed by HPLC for COX-1 and RIA for COX-2. The balance between COX-1/COX-2 and 5-LOX inhibition can be shifted by modifying the substitution pattern of the phenyl moiety at the 6- and 7-position of the pyrrolizine nucleus. Structure-activity relationships are discussed.

Pharmacokinetics of acute and sub-chronic aripiprazole in P-glycoprotein deficient mice

2010

Abstract Background P-glycoprotein (P-gp), an efflux transporter localized in the blood–brain barrier, limits the access of multiple xenobiotics to the central nervous system (CNS). For the new antipsychotic aripiprazole and its active metabolite dehydroaripiprazole differences in disposition in blood and brain were investigated after acute and sub-chronic administration in a P-gp knockout mouse model. Methods Serum and brain concentrations of both drugs were measured at several time points 1–24 h after i.p. injection of 10 mg/kg aripiprazole and after 11 days of sub-chronic administration in several tissues. Moreover, the expression of P-gp was determined by Western blot analysis after sub…

In-vitro test system for the evaluation of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibitors based on a single HPLC run with UV detect…

2001

Objective and Design: The aim of this study was to develop a new, whole-cell test system which is easy to handle and requires a standard equipment for the parallel screening of COX-1 and COX-2 inhibitors.¶Materials: Bovine aortic endothelial cells (BAECs).¶Treatment and methods: Unstimulated bovine aortic coronary endothelial cells (BAECs) were used as a source of COX-1 and BAECs pretreated with ASA (100 μM) and activated with phorbol myristate acetate (PMA) were used as a source of COX-2. The time- and concentration-dependent induction of COX-2 expression in the BAECs was evaluated by a kinetic profile (HPLC analysis) and detected by Western-Blot analysis using polyclonal antibodies agains…

Mildronate treatment improves functional recovery following middle cerebral artery occlusion in rats

2011

Mildronate (3-(2,2,2-trimethylhydrazinium) propionate) is an inhibitor of l-carnitine biosynthesis and an anti-ischemic drug. In the present study, we investigated the effects of mildronate in rats following focal cerebral ischemia. Male Wistar rats were subjected to transient occlusion of the middle cerebral artery (MCAO) for 90min, followed by the intraperitoneal administration of mildronate at doses of 100 and 200mg/kg 2h after reperfusion and then daily for an additional 14days. The beam-walking, rota-rod and cylinder tests were used to assess sensorimotor function, and vibrissae-evoked forelimb-placing and limb-placing tests examined responses to tactile and proprioceptive stimulation.…

Determination of bupivacaine in human plasma by high-performance liquid chromatography.

1984

Comparison of the performance of butanol and pentanol as modifiers in the micellar chromatographic determination of some phenethylamines

2000

Abstract A procedure was developed for the determination of several phenethylamines (amphetamine, arterenol, ephedrine, phenylephrine, phenylpropanolamine, mephentermine, methoxyphenamine, pseudoephedrine and tyramine), using micellar mobile phases of sodium dodecyl sulfate (SDS), a C18 column and UV detection. The drugs were eluted at short retention times with conventional acetonitrile–water or methanol–water mobile phases. In contrast, in the micellar system, they were strongly retained due to association with the surfactant adsorbed on the stationary phase, and needed the addition of butanol or pentanol to be eluted from the column. These modifiers allowed a simple way of controlling th…

Carbonyl reductase 1 is a predominant doxorubicin reductase in the human liver.

2008

A first step in the enzymatic disposition of the antineoplastic drug doxorubicin (DOX) is the reduction to doxorubicinol (DOX-OL). Because DOX-OL is less antineoplastic but more cardiotoxic than the parent compound, the individual rate of this reaction may affect the antitumor effect and the risk of DOX-induced heart failure. Using purified enzymes and human tissues we determined enzymes generating DOX-OL and interindividual differences in their activities. Human tissues express at least two DOX-reducing enzymes. High-clearance organs (kidney, liver, and the gastrointestinal tract) express an enzyme with an apparent Km of approximately 140 microM. Of six enzymes found to reduce DOX, Km valu…